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TGR5-mediated bile acid sensing controls glucose homeostasis.
It is shown here that TGR5 signaling induces intestinal glucagon-like peptide-1 (GLP-1) release, leading to improved liver and pancreatic function and enhanced glucose tolerance in obese mice, and suggested that pharmacological targeting of T GR5 may constitute a promising incretin-based strategy for the treatment of diabesity and associated metabolic disorders. Expand
Targeting bile-acid signalling for metabolic diseases
How the signalling functions of bile acids can be exploited in the development of drugs for obesity, type 2 diabetes, hypertriglyceridaemia and atherosclerosis, as well as other associated chronic diseases such as non-alcoholic steatohepatitis are reviewed. Expand
Manipulation of Brain Kynurenines: Glial Targets, Neuronal Effects, and Clinical Opportunities
Pharmacological agents targeting specific KP enzymes can be used to normalize KP defects, show remarkable efficacy in animal models of central nervous system disorders, and offer novel therapeutic opportunities. Expand
Family-wide chemical profiling and structural analysis of PARP and tankyrase inhibitors
Evaluated small-molecule inhibitors of poly-ADP-ribose polymerase (PARP) family proteins showed that the majority of PARP inhibitors bind multiple targets, providing insight into the design of new inhibitors. Expand
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA), a potent and selective FXR agonist endowed with anticholestatic activity.
6alpha-ethyl-chenodeoxycholic acid (6-ECDCA) was shown to be a very potent and selective FXR agonist and to be endowed with anticholeretic activity in an in vivo rat model of cholestasis. Expand
The nuclear receptor SHP mediates inhibition of hepatic stellate cells by FXR and protects against liver fibrosis.
It is established that FXR ligands might represent a novel therapeutic option to treat liver fibrosis and that SHP binds JunD and inhibits DNA binding of adaptor protein (AP)-1 induced by thrombin. Expand
Structural basis for bile acid binding and activation of the nuclear receptor FXR.
The nuclear receptor FXR is the sensor of physiological levels of enterohepatic bile acids, the end products of cholesterol catabolism. Here we report crystal structures of the FXR ligand bindingExpand
Novel potent and selective bile acid derivatives as TGR5 agonists: biological screening, structure-activity relationships, and molecular modeling studies.
The biological screening of a collection of natural occurring bile acids, bile acid derivatives, and some steroid hormones has resulted in the discovery of new potent and selective T GR5 ligands and a binary classification model of TGR5 activity is developed. Expand
Pharmacological characterization of 1-aminoindan-1,5-dicarboxylic acid, a potent mGluR1 antagonist.
The pharmacological profile of 1-aminoindan-1,5-dicarboxylic acid, a rigid (carboxyphenyl)glycine derivative acting on metabotropic glutamate receptors (mGluRs) is examined to suggest that AIDA is a potent, selective and competitive mGluR1 a antagonist. Expand
TGR5 activation inhibits atherosclerosis by reducing macrophage inflammation and lipid loading.
It is demonstrated that activation of TGR5 in macrophages by 6α-ethyl-23(S)-methylcholic acid (6-EMCA, INT-777), a semisynthetic BA, inhibits proinflammatory cytokine production, an effect mediated by T GR5-induced cAMP signaling and subsequent NF-κB inhibition. Expand